Target intelligence / Profile preview

Bile acid in intestine (BAs)

Target
BAs
Molecular classification
Other (endogenous small molecule/metabolite)
01

Overview

Bile acids are amphipathic steroid-derived metabolites synthesized in the liver from cholesterol and released into the intestine after meals, where they aid in the emulsification and absorption of dietary fats. In the intestine, primary bile acids are modified by the microbiota to secondary bile acids. Beyond their digestive role, bile acids serve as versatile signaling molecules by binding to specific cell-surface and nuclear receptors, notably FXR and GPBAR1, thereby regulating energy metabolism, intestinal motility, immune response, and maintaining gut-liver homeostasis. Clinically, alterations in bile acid composition or their signaling have major roles in conditions such as cholestatic liver diseases, IBD, colorectal cancer, and metabolic syndrome. Bile acid-modifying drugs target these signaling axes for therapeutic benefit, but abnormal bile acid levels can be toxic and are associated with both local and systemic disease processes.

Other names
Bile acidsintestinal bile acidsBAs
02

Mechanism of action

Activation or inhibition of bile acid receptors (e.g., FXR and GPBAR1), thereby modulating metabolic, inflammatory, and proliferative signaling pathways; also, dissolution or modulation of the bile acid pool (as with bile acid therapies for gallstones).

03

Biological functions

Nutrient absorption (emulsification and absorption of dietary lipids)Cholesterol metabolismRegulation of metabolic and immune signaling via bile acid receptorsModulation of intestinal motility and epithelial secretion
04

Disease associations

Liver disease (e.g. cholestasis, primary biliary cholangitis)Inflammatory bowel disease (IBD)Colorectal cancerMetabolic syndrome (e.g. diabetes, obesity)Other (gallstone disease, gut dysbiosis)
05

Safety considerations

Elevated bile acids may be toxic to hepatocytes and intestinal epithelia (bile acid diarrhea, hepatotoxicity)Altered bile acid profiles may promote cancer, inflammation, gut barrier dysfunctionPotential for drug-induced cholestasis with therapeutic bile acids
06

Interacting drugs

Ursodeoxycholic acid (UDCA)

3 more in the full profile.

07

Biomarkers

Serum and fecal bile acid concentrations (indicator of liver/gastrointestinal function)FGF19 (fibroblast growth factor 19, downstream of FXR activation)Expression levels of FXR, GPBAR1 in intestinal biopsies

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